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Corporate Presentation Transforming Discovery Research into Innovative Medicines through Value-Based Partnership CreaGen, Inc. 299 Washington Street Woburn, MA 01801 CreaGen, Inc. Our Goal is to Create A New Generation of Small


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CreaGen, Inc. 299 Washington Street Woburn, MA 01801

Corporate Presentation

Transforming Discovery Research into Innovative Medicines through Value-Based Partnership

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CreaGen, Inc.

Our Goal is to “Create A New Generation of Small Molecules” Through efficient and value-driven partnerships

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Vision

Offer true collaborative services to biotech, pharmaceutical

companies and Federal Research Institutes to accelerate their discovery programs

Build our reputation by exceeding customer expectations

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Established in 2003 Corporate Headquarters: 299 Washington Street, Woburn, MA Scientists: Fifteen experienced chemists total, many with more than ten

years in the pharmaceutical industry

Existing laboratories: ~ 25,000 sq feet: newly expanded in January 2018 Equipment: Waters LC-MS, Varian NMR (300 MHz), Waters auto

purification system, Agilent analytical and Preparative HPLCs, Isco Combi-flash systems, TCAMs for parallel synthesis, Microwave synthesizer, Genevac evaporators, SFC Chiral Chromatography

Library accessibility: online journal subscriptions, SciFinder and

Beilstein/Crossfire access

Resources

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Team

Raj (SB) Rajur, PhD, Founder & CEO

30 Years of academic, industrial and management experience: ArQule, Millipore, Boston College, Northeastern University, Massachusetts General Hospital and Harvard Medical School

Hwa-OK Kim, PhD, Director of Chemistry

30 Years of industrial and management experience: Aurigene Discovery Technologies, Molecumetics, Marion Merrell Dow and New Mexico State University

Venugopal Rao, PhD, Associate Director of Chemistry

20 Years of industrial and project management experience: Pharmacopeia, Microbiotix, Indian Institute of Chemical Technology,

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SAB Team

Norton P. Peet, PhD,

40 Years of industrial and management experience: Aurigene Discovery Technologies, ArQule, Aventis, Marion Merrell Dow, University of Nebraska and Massachusetts Institute of Technology

Robert Perni, PhD,

30 years of industrial and management experience: Vertex Pharmaceuticals, Sirtris Pharmaceuticals, Sterling Winthrop, Avid Therapeutics, Dartmouth College, Northeastern University, University of Rochester

Mark Tebbe, PhD,

30 years of Industrial and management experience: Co-founder of Quench Bio with Atlas Venture and of Arix Bioscience, EIR at Atlas Ventures, Quartet Medicine, Forma Therapeutics, Eli Lilly, Stanford University and University of Notre Dame.

Vinod Patel, PhD,

25 years of industrial experience: Founder, TME therapeutics, Amgen, Kinetix pharmaceuticals, Sanofi-Genzyme and University of Nottingham.

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Medicinal Chemistry:

Small Molecules, High Throughput parallel library synthesis and

purification

Lead Generation and Lead Optimization Conjugation Chemistry, Antibody Drug Conjugates (ADC) Macrocycles and Macrocyclic libraries. Cyclic peptides Nucleosides and Nucleotides, Peptides and Peptide Nucleic Acids

(PNA)

Carbohydrates and unnatural amino acids

Analytical Chemistry:

High Throughput purification and analysis

Expertise

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Why Collaborate with CreaGen

  • CreaGen is a US based company located in Massachusetts
  • CreaGen has an established track record with biotech and large

pharmaceutical organizations

  • Interdisciplinary strengths at CreaGen insure that customers

receive the best value for their investment

CreaGen’s Competitive Advantage: Flexibility, competitive pricing and fast turnaround time Dedicated project teams and segregation of projects Special request capabilities Automated parallel synthesis and separations Customized data input and output Multiple sample delivery formats: dry, in solution, standardized

amounts/concentrations, multiple copies, etc.

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Services

CreaGen performs services that are:

  • -project-based
  • -FTE-based
  • -collaboration-based
  • Medicinal chemistry and lead optimization
  • Building blocks/scaffolds/key intermediates
  • Customer tailored focused libraries
  • High throughput purification and QC solutions

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Case studies: Representative Examples

CS I: Multinational Pharma (Oncology) : Lead Optimization Project requirements:

  • Design and optimize leads, synthesize novel analogs of the leads for weekly screening
  • Provide all medicinal chemistry expertise to client in designing new analogs and libraries.

Explore new synthetic routes. Accomplishments:

  • 3-Year collaboration FTE based contract
  • Provided more than 600 compounds and many novel scaffolds during the tenure of the
  • program. True extension of customer’s chemistry program

CS II: Multinational Pharma : Antibody Drug Conjugates (ADC) Project requirements:

  • Design and synthesize novel linkers. Conjugate novel small molecules and drug candidates

to linkers. Introduce reactive functionalities on the linker to conjugate to antibodies.

  • Provide conjugation chemistry expertise to client. Synthesize libraries of small molecules.

Explore new synthetic routes. Accomplishments:

  • 2-Year FTE based collaboration
  • Provided several conjugates to client for screening. Developed several novel hydrophilic

molecules to conjugate to antibodies to minimize aggregation. True extension of customer’s ADC program

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CS III: Biotech. (Anti-infective): NIH & funded projects: (CreaGen -subcontractor)

Project Requirements:

  • Design and synthesize novel scaffolds and develop new and efficient routes

for the synthesis

  • Provide multi-gram quantities of final compounds for in vivo tox studies with

aggressive timeline

  • Perform process development for multi-step synthesis of scaffolds and lead

molecules

Accomplishments:

  • Five year collaborations: Provided 20 scaffolds and associated libraries and several

multigram scale non-GMP compounds for in vivo tox studies CS IV: Biotech. (Anti-infective): Lead Optimization Project requirements:

  • Function as medicinal chemistry department
  • Provide all medicinal chemistry expertise to client in designing new analogs
  • Develop SAR and interpret weekly screening results with client and suggest new ideas

Accomplishments:

  • Expanded collaboration to 8 FTEs: company sold to Biota Australia

Case studies: Representative Examples

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Case study: Representative Examples

CS V: NIH a) NCATS: Synthesis of commercial preclinical candidate Project requirements and accomplishments:

  • Synthesis of 10 grams of ERK inhibitor
  • Completed the synthesis within budget and delivered the compound on time.

b) NCI: Synthesis of commercial preclinical compound Project requirements and accomplishments:

  • Synthesis of 10 grams of MMP inhibitor
  • Completed the synthesis and delivered the product on time

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Case studies: Representative Examples

CS VI: Small Biotech (Diabetes): Lead Optimization Project requirements:

  • Function as de facto medicinal chemistry department
  • Provide all medicinal chemistry expertise starting with design discussion, literature

searches, hit-to-lead evaluation, SAR studies, lead optimization, identification and selection of high-value preclinical candidates Accomplishments:

  • Generated IP for their AMPK program in seven months
  • Provided a nanomolar compound and several backup compounds with activities in the

micromolar range

  • Expanded to 4 FTEs
  • Project grew as milestones were delivered and the program was licensed to

Debiophama

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Small Molecule Library Synthesis (examples)

Partner Biotech Multinational Pharma Small Biotech

Project

Hit to Lead Hit to Lead Optimization Exploratory to Hit/Lead

Duration

2.5 years 3.5years 2 years

FTEs involved

1~1.5 2~4 2~4 # of compounds 750 600 2500

library synthesis: Synthetic steps

1~3 6~7 5~6

Library synthesis Method

solution phase parallel synthesis solution phase parallel synthesis solution phase parallel synthesis

Qty of compounds

10-20mg Ave 50mg Ave 20mg

Qty for scaffolds /intermediates

2g to 50g 1g to 100g 1g to 30g

Purity

90 to 98% 90 to 98% 90 to 98%

Analytical data 1H NMR, 13C NMR, 2D NMR, LC-MS, HPLC, elemental analysis, HRMS etc 1H NMR, 13C NMR, LC-MS, HPLC, elemental analysis, HRMS etc 1H NMR, 13C NMR, LC-MS, HPLC, elemental analysis HRMS etc Resulted in

Lead Optimization Filed patent: _ Lead Optimization Filed patent: _ Lead Optimization 14

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Partner

Therapeutic Area Lead Discovery Lead Optimization Clinical Candidate Phase I, II & III

Multinational Pharma Cancer Biotech Diabetes Biotech Anti-infective Biotech Anti-infective Biotech Cancer Biotech Cancer Biotech CNS Asian Biotech Cancer European Pharma Diabetes 15

CreaGen Synthesized Compounds: Various Stages in Partner Programs

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CreaGen Infrastructure & Equipment

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CreaGen parallel synthesis platform

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CreaGen parallel synthesis work stations

  • 1, 2 and 4 position

heater/shakers

  • Heating up to 150ºC
  • Variable speed vortexing
  • Timed shutoff
  • Integration with automation

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Synthesis work stations: cont’d Parallel synthesizer High speed evaporator GeneVac (EZ2)

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CreaGen purification work stations Mass directed purification Chiral purification: SFC

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CreaGen analytical work stations CreaGen analytical work stations

Varian, 300 MHz NMR

TQ- LCMS

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CreaGen: LCMS

The picture can't be displayed.

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Summary

Competitive pricing Excellent communication Quality services On-time delivery Customer satisfaction

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